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GIBH-130 is a neuroinflammation inhibitor, with IC50 value of 3.4 nM for suppressing the IL-1β secretion by activated microglia. GIBH-130 exhibited comparable in vivo efficacy of cognitive impairment relief to donepezil and memantine respectively in both β amyloid-induced and APP/PS1 double transgenic Alzheimer's murine models at a substantially lower dose (0.25 mg/kg). GIBH-130 is found to be orally bioavailable in rats, with 74.91% bioavailability and 4.32 h half-life.
| Molecular Weight | 360.41 |
| Formula | C20H20N6O |
| CAS Number | 1252608-59-5 |
| Solubility (25°C) | DMSO 44 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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